EGFR/HER2/DHFR-IN-2 (Compound 4b) is an inhibitor of EGFR , HER2 , and DHFR ( IC 50 : 0.248, 0.156, 0.138 μM respectively). EGFR/HER2/DHFR-IN-2 has anticancer activities against a panel of cancer cells ( IC 50 : 9.14, 7.33, 14.18, 24.87, 20.07, 6.16 μM for Hep G2, HeLa, HEp-2, HCT 116, PC-3, MCF7 cells). EGFR/HER2/DHFR-IN-2 reduce breast cancer tumor growth.